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Inhibitor by virtue of interaction of P53-MDM2 and applications of inhibitor

A technology of P53-MDM2 and inhibitor, which is applied to the inhibitor of P53-MDM2 interaction and its application field to achieve a good effect of promoting apoptosis

Inactive Publication Date: 2014-12-10
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term clinical practice has proved the safety of Ganoderma lucidum and its components, and the screening of P53-MDM2 interaction inhibitors from Ganoderma lucidum has not been reported

Method used

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  • Inhibitor by virtue of interaction of P53-MDM2 and applications of inhibitor
  • Inhibitor by virtue of interaction of P53-MDM2 and applications of inhibitor
  • Inhibitor by virtue of interaction of P53-MDM2 and applications of inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Toxic effect of GA-T on 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells not expressing P53 protein

[0051] Take 4 parts of GA-T with a purity greater than 99%, and dilute them with DMSO (dimethyl sulfoxide, analytical grade, Shanghai Sinopharm Chemical Reagent Co., Ltd.) to concentrations of 8.5 μg / ml, 10 μg / ml, 25 μg / ml, 50 μg / ml.

[0052] Using thiazolium blue (hereinafter referred to as MTT, analytically pure, Shanghai Sinopharm Chemical Reagent Co., Ltd.) rapid colorimetric method to determine the effect of the above four different concentrations of GA-T on two kinds of 95-D lung cancer cells expressing P53 protein and non-expressing P53 protein Toxic effects of H1299 lung cancer cells.

[0053] Cells in logarithmic growth phase (10 6 cell.ml -1 ) inoculated in 96-well culture plate, 0.2ml per well, and then added the above four different concentrations of GA-T for treatment, each concentration was parallel to 4 wells, the final conce...

Embodiment 2

[0055] Inhibitory effect of GA-Me treatment at different concentrations and times on 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells not expressing P53 protein

[0056] The purity of GA-Me was more than 99%, and it was diluted with DMSO to the desired concentration. The toxic effect of GA-Me on 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells not expressing P53 protein was determined by thiazolium blue (MTT) rapid colorimetric method.

[0057] 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells (106cell.ml-1) not expressing P53 protein in the logarithmic growth phase were inoculated in a 96-well culture plate, 0.2ml per well, and the two different cells were respectively Add GA-Me at a final concentration of 16 μg / ml and 80 μg / ml, parallel 4 wells for each concentration, and the final concentration of DMSO in each well is less than 0.1%, and add an equal volume of RPMI1640 cell culture medium (Saiye Suz...

Embodiment 3

[0059] GA-X, GA-Me, GA-Y, GA-T, GA-F Induction of apoptosis in 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells not expressing P53 protein

[0060]95-D lung cancer cells expressing P53 protein in the logarithmic growth phase and H1299 lung cancer cells not expressing P53 protein were cultured for 4 hours, and then diluted with DMSO to obtain 50 μg / mL of the above GA-X, GA-Me, GA-Y, GA- After T and GA-F were fully reacted for 8 hours, digested with trypsin, collected 95-D lung cancer cells expressing P53 protein and H1299 lung cancer cells not expressing P53 protein by centrifugation (1500 rpm × 10min), PBS (sodium chloride ( NaCl), 8g / L; Potassium chloride (KCl), 0.2g / L; Disodium hydrogen phosphate (Na2HPO4), 1.44g / L; Potassium dihydrogen phosphate (KH2PO4), 0.24g / L, adjusted to pH 7.4, high pressure steam sterilization, stored at room temperature) and washed twice, adjust the concentrations of 95-D lung cancer cells expressing P53 protein and H1299 ...

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Abstract

The invention discloses an inhibitor by virtue of interaction of P53-MDM2 and applications of the inhibitor. The inhibitor by virtue of interaction of P53-MDM2 is ganoderic acid X, ganoderic acid Me, ganoderic acid Y, ganoderic acid T or ganoderic acid F or a composition formed by combining one of ganoderic acid X, ganoderic acid Me, ganoderic acid Y, ganoderic acid T and ganoderic acid F with pharmacologically acceptable additive components. The inhibitor by virtue of interaction of P53-MDM2, disclosed by the invention, is applied to promotion of the apoptosis of tumor cells and particularly applied to promotion of the apoptosis of the 95-D lung cancer cells expressing P53 proteins or H1299 lung cancer cells not expressing the P53 proteins; the inhibitor by virtue of interaction of P53-MDM2, disclosed by the invention, has the effects of remarkably inhibiting the activity of MDM2 in human malignant lung cancer cells, thereby inhibiting the degradation of the P53 proteins and further promoting the apoptosis of the tumor cells containing P53.

Description

technical field [0001] The invention relates to an inhibitor of P53-MDM2 interaction and its application in inducing tumor cell apoptosis mediated by P53. Background technique [0002] With changes in factors affecting the occurrence and development of tumors, such as lifestyle, environmental conditions, and population aging, the incidence of tumors in my country has shown a clear upward trend since the 1970s, and has become the leading cause of death among urban and rural residents. The common feature of tumors is that they have the ability to proliferate indefinitely due to the defect of normal cell apoptosis system leading to apoptosis disorder (Carcinogenesis, 21:485, 2000). Therefore, targeting negative regulators that play a central role in directly inhibiting apoptosis in cancer cells represents a promising therapeutic strategy for the design of new anticancer drugs. [0003] Ganoderma lucidum is a traditional medicinal fungus. The Pharmacopoeia of the People's Repub...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P35/00
Inventor 唐文王雨蔷孙培龙欧阳晶晶
Owner SHANGHAI INST OF TECH
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